Assay Detail
Binding
CHEMBL4001847
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Displacement of [3H]-S-citalopram from human SERT primary site (S1) expressed in African green monkey COS7 cell membranes after 2 hrs by microbeta scintillation counting method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
X-ray structure based evaluation of analogs of citalopram: Compounds with increased affinity and selectivity compared with R-citalopram for the allosteric site (S2) on hSERT.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.55 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1508 | ESCITALOPRAM | 4.0 | 1 | 8.00 |
| CHEMBL4083258 | — | — | 1 | 7.12 |
| CHEMBL4097442 | — | — | 1 | 6.80 |
| CHEMBL4100796 | — | — | 1 | 6.72 |
| CHEMBL4093087 | — | — | 1 | 6.55 |
| CHEMBL4070256 | — | — | 1 | 5.96 |
| CHEMBL4065415 | — | — | 1 | 5.64 |
| CHEMBL4074032 | — | — | 1 | 5.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1508 | ESCITALOPRAM | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4083258 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4097442 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4100796 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4093087 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4070256 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4065415 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4074032 | — | IC50 | = | 2400.0 | nM | 5.62 |